Recent progress in sustained/controlled oral delivery of captopril: an overview

Area of Science:

• Pharmaceutical Sciences
• Drug Delivery Systems

Background:

• Captopril is a widely used antihypertensive and heart failure medication.
• Developing oral sustained or controlled-release dosage forms for captopril presents significant challenges.
• These challenges stem from captopril's high water solubility and instability in the alkaline intestinal environment.

Purpose of the Study:

• To review the research and development of oral sustained/controlled-release captopril formulations.
• To highlight the difficulties and successes in creating these advanced drug delivery systems.
• To assess the current state of clinical validation for existing captopril formulations.

Main Methods:

• Literature review of published research on captopril controlled-release formulations.
• Analysis of formulation strategies aimed at overcoming solubility and stability issues.
• Evaluation of in vitro data and available clinical evidence for developed formulations.

Main Results:

• Numerous attempts have been made to develop sustained/controlled-release captopril formulations.
• Key challenges include managing high water solubility and intestinal degradation.
• While some formulations have been patented, clinical efficacy data is often limited, relying primarily on in vitro results.

Conclusions:

• The development of effective oral sustained/controlled-release captopril remains a complex area of pharmaceutical research.
• Overcoming formulation hurdles requires innovative approaches to drug solubility and stability.
• Further clinical studies are needed to validate the efficacy of developed captopril formulations.